Impact of the aryl substituent kind and distance from pyrimido[2,1-f]purindiones on the adenosine receptor selectivity and antagonistic properties

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Abstract

Adenosine receptor (AR) antagonists belong to two major groups of compounds: xanthines and non-xanthines. Recently several annelated xanthine derivatives have been described as selective A1, A2A, A2B and A3 ARs antagonists. Contrary to dipropyl derivatives, in the group of dimethyl (un)substituted arylalkyl pyrimido[2,1-f]purindiones selective mainly adenosine A2A receptor antagonists were identified. Their activity depended on aryl substitution and its distance from pyrimido[2,1-f]purindione.

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Acknowledgements

This study was supported in part by the Polish State Committee for Scientific Research (Grant No 6 P05F 024 21), and by the Deutsche Forschungsgemeinschaft (GRK-677). The authors are grateful to Professor James P. Stables for providing anticonvulsant test data through the Antiepileptic Drug Development Program, National Institutes of Health, Bethesda, Maryland, USA.

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